A new series of compds., in which the 2-amino-4-methoxyphenyl ring of a phenstatin analog was replaced with 2- or 3-amino-benzoheterocycles, was synthesized and evaluated for antiproliferative activity and inhibition of colchicine binding. The lack of activity of 3',4'-dimethoxy- and 4'-methoxy-benzoyl derivs. indicates that the 3',4',5'-trimethoxybenzoyl moiety is crit. for the activity. Two compds. (I and II), displayed potent antiproliferative activity, with IC50 values ranging from 25 to 100 nM against a variety of cancer cell lines. Deriv. II was more active than CA-4 as an inhibitor of tubulin polymn. The results demonstrated that the antiproliferative activity was correlated with inhibition of tubulin polymn.

Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles

ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;IACONINOTO, Antonietta;PRETI, Delia;AGHAZADEH TABRIZI, Mojgan;FRUTTAROLO, Francesca;
2005

Abstract

A new series of compds., in which the 2-amino-4-methoxyphenyl ring of a phenstatin analog was replaced with 2- or 3-amino-benzoheterocycles, was synthesized and evaluated for antiproliferative activity and inhibition of colchicine binding. The lack of activity of 3',4'-dimethoxy- and 4'-methoxy-benzoyl derivs. indicates that the 3',4',5'-trimethoxybenzoyl moiety is crit. for the activity. Two compds. (I and II), displayed potent antiproliferative activity, with IC50 values ranging from 25 to 100 nM against a variety of cancer cell lines. Deriv. II was more active than CA-4 as an inhibitor of tubulin polymn. The results demonstrated that the antiproliferative activity was correlated with inhibition of tubulin polymn.
2005
Romagnoli, Romeo; Baraldi, Pier Giovanni; Jung, Mk; Iaconinoto, Antonietta; Carrion, Md; Remusat, V; Preti, Delia; AGHAZADEH TABRIZI, Mojgan; Fruttarolo, Francesca; DE CLERCQ, E; Balzarini, J; Hamel, E.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/516948
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